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| {{STRUCTURE_1t5z| PDB=1t5z | SCENE= }} | | {{STRUCTURE_1t5z| PDB=1t5z | SCENE= }} |
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| '''Crystal Structure of the Androgen Receptor Ligand Binding Domain (LBD) with DHT and a peptide derived from its physiological coactivator ARA70'''
| | ===Crystal Structure of the Androgen Receptor Ligand Binding Domain (LBD) with DHT and a peptide derived from its physiological coactivator ARA70=== |
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| ==Overview==
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| Androgens drive sex differentiation, bone and muscle development, and promote growth of hormone-dependent cancers by binding the nuclear androgen receptor (AR), which recruits coactivators to responsive genes. Most nuclear receptors recruit steroid receptor coactivators (SRCs) to their ligand binding domain (LBD) using a leucine-rich motif (LXXLL). AR is believed to recruit unique coactivators to its LBD using an aromatic-rich motif (FXXLF) while recruiting SRCs to its N-terminal domain (NTD) through an alternate mechanism. Here, we report that the AR-LBD interacts with both FXXLF motifs and a subset of LXXLL motifs and that contacts with these LXXLL motifs are both necessary and sufficient for SRC-mediated AR regulation of transcription. Crystal structures of the activated AR in complex with both recruitment motifs reveal that side chains unique to the AR-LBD rearrange to bind either the bulky FXXLF motifs or the more compact LXXLL motifs and that AR utilizes subsidiary contacts with LXXLL flanking sequences to discriminate between LXXLL motifs.
| | The line below this paragraph, {{ABSTRACT_PUBMED_15563469}}, adds the Publication Abstract to the page |
| | (as it appears on PubMed at http://www.pubmed.gov), where 15563469 is the PubMed ID number. |
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| | {{ABSTRACT_PUBMED_15563469}} |
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| ==About this Structure== | | ==About this Structure== |
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| [[Category: Webb, P.]] | | [[Category: Webb, P.]] |
| [[Category: Androgen receptor ligand binding domain ara70 crystal structure coactivator]] | | [[Category: Androgen receptor ligand binding domain ara70 crystal structure coactivator]] |
| ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 09:34:04 2008'' | | |
| | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 18:30:28 2008'' |